MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 464624 | Name: NEO2734
Featured New

Description:

WARNING: This product is for research use only, not for human or veterinary use.

NEO2734 is a novel, orally active, and selective dual inhibitor targeting both BET bromodomains and the histone acetyltransferases CBP/p300. Binding assays have demonstrated that NEO2734 exhibits dissociation constants (K_d) of 6 nM for BRD4, 19 nM for CBP, and 31 nM for p300, indicating high affinity for these targets. The compound effectively reduces the transcription of oncogenes, such as MYC, with an EC_50 of 14 nM. In vitro studies have shown that NEO2734 inhibits the proliferation of various cancer cell lines, including those derived from lymphomas, leukemias, and prostate cancer. In vivo, NEO2734 has demonstrated significant antitumor activity, leading to tumor regression and extended survival in mouse models of NUT midline carcinoma.

Chemical Structure

NEO2734
NEO2734
CAS#2081072-29-7

Theoretical Analysis

MedKoo Cat#: 464624

Name: NEO2734

CAS#: 2081072-29-7

Chemical Formula: C22H24F3N3O3

Exact Mass: 435.1770

Molecular Weight: 435.45

Elemental Analysis: C, 60.68; H, 5.56; F, 13.09; N, 9.65; O, 11.02

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 2 Weeks
25mg USD 150.00 2 Weeks
50mg USD 250.00 2 Weeks
100mg USD 450.00 2 Weeks
1g USD 2,950.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
No Data
Synonym
NEO2734; NEO 2734; NEO-2734;
IUPAC/Chemical Name
1,3-dimethyl-5-(2-(tetrahydro-2H-pyran-4-yl)-1-(2-(trifluoromethoxy)ethyl)-1H-benzo[d]imidazol-6-yl)pyridin-2(1H)-one
InChi Key
KPWWFNXRLAAREN-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H24F3N3O3/c1-14-11-17(13-27(2)21(14)29)16-3-4-18-19(12-16)28(7-10-31-22(23,24)25)20(26-18)15-5-8-30-9-6-15/h3-4,11-13,15H,5-10H2,1-2H3
SMILES Code
O=C1C(C)=CC(C2=CC=C3C(N(CCOC(F)(F)F)C(C4CCOCC4)=N3)=C2)=CN1C
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 435.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Wu X, Zhang X, Tang S, Wang Y. The important role of the histone acetyltransferases p300/CBP in cancer and the promising anticancer effects of p300/CBP inhibitors. Cell Biol Toxicol. 2025 Jan 17;41(1):32. doi: 10.1007/s10565-024-09984-0. PMID: 39825161; PMCID: PMC11742294. 2: Verbeke S, Bourdon A, Lafon M, Chaire V, Frederic B, Naït Eldjoudi A, Derieppe MA, Giles F, Italiano A. Dual inhibition of BET and EP300 has antitumor activity in undifferentiated pleomorphic sarcomas and synergizes with ferroptosis induction. Transl Oncol. 2025 Feb;52:102236. doi: 10.1016/j.tranon.2024.102236. Epub 2024 Dec 15. PMID: 39681067; PMCID: PMC11713734. 3: Choo N, Keerthikumar S, Ramm S, Ashikari D, Teng L, Niranjan B, Hedwards S, Porter LH, Goode DL, Simpson KJ, Taylor RA, Risbridger GP, Lawrence MG. Co- targeting BET, CBP, and p300 inhibits neuroendocrine signalling in androgen receptor-null prostate cancer. J Pathol. 2024 Jun;263(2):242-256. doi: 10.1002/path.6280. Epub 2024 Apr 5. PMID: 38578195. 4: Strachowska M, Robaszkiewicz A. Characteristics of anticancer activity of CBP/p300 inhibitors - Features of their classes, intracellular targets and future perspectives of their application in cancer treatment. Pharmacol Ther. 2024 May;257:108636. doi: 10.1016/j.pharmthera.2024.108636. Epub 2024 Mar 22. PMID: 38521246. 5: Sun R, Yan B, Li H, Ding D, Wang L, Pang J, Ye D, Huang H. Androgen Receptor Variants Confer Castration Resistance in Prostate Cancer by Counteracting Antiandrogen-Induced Ferroptosis. Cancer Res. 2023 Oct 2;83(19):3192-3204. doi: 10.1158/0008-5472.CAN-23-0285. PMID: 37527336; PMCID: PMC10543964. 6: Kuang C, Tong J, Ermine K, Cai M, Dai F, Hao S, Giles F, Huang Y, Yu J, Zhang L. Dual inhibition of BET and HAT/p300 suppresses colorectal cancer via DR5- and p53/PUMA-mediated cell death. Front Oncol. 2022 Oct 12;12:1018775. doi: 10.3389/fonc.2022.1018775. PMID: 36313707; PMCID: PMC9599411. 7: Ji D, Shang G, Wei E, Jia Y, Wang C, Zhang Q, Zeng L. Targeting CDCP1 gene transcription coactivated by BRD4 and CBP/p300 in castration-resistant prostate cancer. Oncogene. 2022 Jun;41(23):3251-3262. doi: 10.1038/s41388-022-02327-5. Epub 2022 May 5. PMID: 35513563. 8: van Gils N, Martiañez Canales T, Vermue E, Rutten A, Denkers F, van der Deure T, Ossenkoppele GJ, Giles F, Smit L. The Novel Oral BET-CBP/p300 Dual Inhibitor NEO2734 Is Highly Effective in Eradicating Acute Myeloid Leukemia Blasts and Stem/Progenitor Cells. Hemasphere. 2021 Jul 8;5(8):e610. doi: 10.1097/HS9.0000000000000610. PMID: 34258514; PMCID: PMC8265862. 9: He Y, Wei T, Ye Z, Orme JJ, Lin D, Sheng H, Fazli L, Jeffrey Karnes R, Jimenez R, Wang L, Wang L, Gleave ME, Wang Y, Shi L, Huang H. A noncanonical AR addiction drives enzalutamide resistance in prostate cancer. Nat Commun. 2021 Mar 9;12(1):1521. doi: 10.1038/s41467-021-21860-7. PMID: 33750801; PMCID: PMC7943793. 10: Zhou Y, Jin X, Ma J, Ding D, Huang Z, Sheng H, Yan Y, Pan Y, Wei T, Wang L, Wu H, Huang H. HDAC5 Loss Impairs RB Repression of Pro-Oncogenic Genes and Confers CDK4/6 Inhibitor Resistance in Cancer. Cancer Res. 2021 Mar 15;81(6):1486-1499. doi: 10.1158/0008-5472.CAN-20-2828. Epub 2021 Jan 8. PMID: 33419772. 11: Ryan KR, Giles F, Morgan GJ. Targeting both BET and CBP/EP300 proteins with the novel dual inhibitors NEO2734 and NEO1132 leads to anti-tumor activity in multiple myeloma. Eur J Haematol. 2021 Jan;106(1):90-99. doi: 10.1111/ejh.13525. Epub 2020 Oct 22. PMID: 32997383. 12: Spriano F, Gaudio E, Cascione L, Tarantelli C, Melle F, Motta G, Priebe V, Rinaldi A, Golino G, Mensah AA, Aresu L, Zucca E, Pileri S, Witcher M, Brown B, Wahlestedt C, Giles F, Stathis A, Bertoni F. Antitumor activity of the dual BET and CBP/EP300 inhibitor NEO2734. Blood Adv. 2020 Sep 8;4(17):4124-4135. doi: 10.1182/bloodadvances.2020001879. PMID: 32882003; PMCID: PMC7479962. 13: Morrison-Smith CD, Knox TM, Filic I, Soroko KM, Eschle BK, Wilkens MK, Gokhale PC, Giles F, Griffin A, Brown B, Shapiro GI, Zucconi BE, Cole PA, Lemieux ME, French CA. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 Jul;19(7):1406-1414. doi: 10.1158/1535-7163.MCT-20-0087. Epub 2020 May 5. PMID: 32371576. 14: Yan Y, Ma J, Wang D, Lin D, Pang X, Wang S, Zhao Y, Shi L, Xue H, Pan Y, Zhang J, Wahlestedt C, Giles FJ, Chen Y, Gleave ME, Collins CC, Ye D, Wang Y, Huang H. The novel BET-CBP/p300 dual inhibitor NEO2734 is active in SPOP mutant and wild-type prostate cancer. EMBO Mol Med. 2019 Nov 7;11(11):e10659. doi: 10.15252/emmm.201910659. Epub 2019 Sep 26. PMID: 31559706; PMCID: PMC6835201.

View History

Pelrinone Free Base

Pelrinone Free Base